132550-73-3Relevant academic research and scientific papers
2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
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Page/Page column 27, (2010/11/08)
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hy
Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors
Albrecht, Sebastien,Defoin, Albert,Salomon, Emmanuel,Tarnus, Celine,Wetterholm, Anders,Haeggstroem, Jasper Z.
, p. 7241 - 7257 (2007/10/03)
Racemic derivatives of 3-amino-2-tetralone were synthesised and evaluated for their ability to inhibit metallo-aminopeptidase activities. New compounds substituted in position 2 by methyl ketone, substituted oximes or hydroxamic acids as well as heterocyclic derivatives were evaluated against representative members of zinc-dependent aminopeptidases: leucine aminopeptidase (E.C. 3.4.11.1), aminopeptidase-N (E.C. 3.4.11.2), Aeromonas proteolytica aminopeptidase (E.C. 3.4.11.10), and the aminopeptidase activity of leukotriene A4 hydrolase (E.C. 3.3.2.6). Several compounds showed Ki values in the low micromolar range against the 'one-zinc' aminopeptidases, while most of them were rather poor inhibitors of the 'two-zinc' enzymes. This interesting selectivity profile may guide the design of new, specific inhibitors of target mammalian aminopeptidases with one active site zinc.
